2. GPCR/G Protein
  3. P2Y Receptor
  4. Diquafosol tetrasodium

Diquafosol tetrasodium  (Synonyms: INS365)

Cat. No.: HY-B0606 Purity: ≥99.0%
COA Handling Instructions

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Diquafosol tetrasodium is a P2Y2 receptor agonist that stimulates fluid and mucin secretion on the ocular surface, as a topical treatment of dry eye disease.

For research use only. We do not sell to patients.

Diquafosol tetrasodium Chemical Structure

Diquafosol tetrasodium Chemical Structure

CAS No. : 211427-08-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
 USD 124 In-stock
Solution
10 mM * 1 mL in Water USD 124 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 128 In-stock
50 mg USD 400 In-stock
100 mg USD 600 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 4 publication(s) in Google Scholar

Diquafosol tetrasodium Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Diquafosol tetrasodium is a P2Y2 receptor agonist that stimulates fluid and mucin secretion on the ocular surface, as a topical treatment of dry eye disease.

IC50 & Target

P2Y2 Receptor

 

In Vitro

Cell viability significantly decreased after treatment with 30% diluted diquafosol for 1 hour and 6 hours after treatment with 10% and 20% diluted diquafosol. Twenty-four hours after wounding monolayers, 3% diquafosol, and 0.3% HCECs exhibits significantly more wound healing than the control[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Diquafosol tetrasodium Related Antibodies
In Vivo

In a rat dry eye model, the P2Y2 agonist diquafosol tetrasodium is found to improve surface health, based on increases in tear fluid secretion, corneal epithelial resistance, and release of glycoprotein-containing moieties from goblet cells. Beginning at 2 weeks and continuing for an additional 2 weeks, maximal declines in dye penetrance of approximately 50% occurred with doses of diquafosol tetrasodium as low as 1%[2]. INS365 significantly suppresses corneal damage at concentrations of more than 0.1% w/v[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

878.23

Formula

C18H22N4Na4O23P4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@@H](O)[C@H](N(C(N2)=O)C=CC2=O)O[C@@H]1COP(OP(OP(OP(OC[C@@H]3[C@@H](O)[C@@H](O)[C@H](N4C(NC(C=C4)=O)=O)O3)(O[Na])=O)(O[Na])=O)(O[Na])=O)(O[Na])=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (113.87 mM; Need ultrasonic)

DMSO : 1 mg/mL (1.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1387 mL 5.6933 mL 11.3865 mL
5 mM 0.2277 mL 1.1387 mL 2.2773 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (113.87 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥99.0%

COA (262 KB) HNMR (192 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

The viabilities of human corneal epithelial cells (HCECs) are determined using a MTT assay. Cells are subconfluent Diquafosol (100 mL diluted 10%, 20%, or 30%) or DMEM (100 mL) is added to controls. After 1, 6, and 24 h, plates are washed three times with PBS to remove the drugs. Cell viabilities are evaluated after incubating for 24 h. MTT is then added to each well. Samples are incubated in the dark for 4 h at 37oC, and media are then removed. Precipitates are resuspended in DMSO. Absorbances are measured on a plate reader at 570 nm[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Rats: An SD rat dry eye model is used in which exorbital lacrimal gland extirpation decreased the Schirmer test score by at least 50%. After 8 weeks, when significant increases occurred in corneal epithelial permeability, INS365-containing eye drops are applied six times daily for the next 4 weeks at concentrations from 0.03% to 3.0%. Corneal barrier function is evaluated based on measurements with a modified anterior fluorometer of fluorescein penetrance at 1, 2, and 4 weeks after initial application. After INS365 application, the periodic acid–Schiff reagent (PAS)–stained area is evaluated in histologic sections of the tarsal and bulbar conjunctiva[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.1387 mL 5.6933 mL 11.3865 mL 28.4663 mL
H2O 5 mM 0.2277 mL 1.1387 mL 2.2773 mL 5.6933 mL
10 mM 0.1139 mL 0.5693 mL 1.1387 mL 2.8466 mL
15 mM 0.0759 mL 0.3796 mL 0.7591 mL 1.8978 mL
20 mM 0.0569 mL 0.2847 mL 0.5693 mL 1.4233 mL
25 mM 0.0455 mL 0.2277 mL 0.4555 mL 1.1387 mL
30 mM 0.0380 mL 0.1898 mL 0.3796 mL 0.9489 mL
40 mM 0.0285 mL 0.1423 mL 0.2847 mL 0.7117 mL
50 mM 0.0228 mL 0.1139 mL 0.2277 mL 0.5693 mL
60 mM 0.0190 mL 0.0949 mL 0.1898 mL 0.4744 mL
80 mM 0.0142 mL 0.0712 mL 0.1423 mL 0.3558 mL
100 mM 0.0114 mL 0.0569 mL 0.1139 mL 0.2847 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Diquafosol tetrasodium Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Diquafosol tetrasodium211427-08-6INS365INS 365INS-365P2Y ReceptorInhibitorinhibitorinhibit

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